Development of a Process to a 4-Arylated 2-Methylisoquinolin-1(2H)-one for the Treatment of Solid Tumors: Lessons in Ortho-Bromination, Selective Solubility, Pd Deactivation, and Form Control

已完结 10 由大欣发布于 2024/9/18 11:00:48

DOI:10.1021/acs.oprd.2c00057
作者：David N. Primer*,?Kelvin Yong,?Antonio Ramirez,?Matthew Kreilein*,?Antonio C. Ferretti,?Antonio M. Ruda,?Nadia Fleary-Roberts,?Jonathan D. Moseley,?Sian M. Forsyth,?Graham R. Evans and John F. Travers
文献类型：期刊论文
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American Chemical Society (ACS)

Abstract：We here present an optimized, scalable synthesis of bromodomain and extra-terminal (BET) inhibitor BMS-986378 (CC-90010). The original route and process 1A was 7 steps with 33.8% yield and f

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